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编 号：F177681
分子式：C12H22ClN3O5S3
分子量：419.97
分子式：C12H22ClN3O5S3
分子量：419.97
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CAS No: 150937-43-2
产品详情
生物活性：
Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with an IC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research.
体内研究：
Brinzolamide (7.5 mg or 12 mg) hydrochloride implanted in a silicone matrix is extremely well tolerated and provides sustained release of brinzolamide and significant reduction in intraocular pressure (IOP) for up to 28 days with no adverse effects or signs of toxicity in normotensive NZW rabbits.The pharmacokinetic parameters of Brinzolamide hydrochloride in rabbits.Intracameral Administration (4.5 mg)Intracameral Administration (4.5 mg)Topical Administration (500 mg)Topical Administration (500 mg)
PK ParametersAqueous HumorIris-Ciliary BodyAqueous HumorIris-Ciliary Body
Tmax (h)0.080.510.25
Cmax (ng/mL, ng/g)11,05019644081245
Terminal t1/2 (h)3.413213.6
AUC0-24h (h*ng/mL, h*ng/g)17,7807725189611414
AUC0-∞ (h*ng/mL, h*ng/g)17,8368839195516628
Dose-normalized AUC0-∞ (h*/mL, h*/g)420.0040.03
Animal Model:Rabbits
Dosage:7.5 mg, 12 mg
Administration:Implant placed in the episcleral space
Result:Resulted in a significant IOP reduction of 4.6 mmHg on days 10-28, with concentrations of 12 mg.
Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with an IC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research.
体内研究：
Brinzolamide (7.5 mg or 12 mg) hydrochloride implanted in a silicone matrix is extremely well tolerated and provides sustained release of brinzolamide and significant reduction in intraocular pressure (IOP) for up to 28 days with no adverse effects or signs of toxicity in normotensive NZW rabbits.The pharmacokinetic parameters of Brinzolamide hydrochloride in rabbits.Intracameral Administration (4.5 mg)Intracameral Administration (4.5 mg)Topical Administration (500 mg)Topical Administration (500 mg)
PK ParametersAqueous HumorIris-Ciliary BodyAqueous HumorIris-Ciliary Body
Tmax (h)0.080.510.25
Cmax (ng/mL, ng/g)11,05019644081245
Terminal t1/2 (h)3.413213.6
AUC0-24h (h*ng/mL, h*ng/g)17,7807725189611414
AUC0-∞ (h*ng/mL, h*ng/g)17,8368839195516628
Dose-normalized AUC0-∞ (h*/mL, h*/g)420.0040.03
Animal Model:Rabbits
Dosage:7.5 mg, 12 mg
Administration:Implant placed in the episcleral space
Result:Resulted in a significant IOP reduction of 4.6 mmHg on days 10-28, with concentrations of 12 mg.
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